一种具有认知增强作用的药物α-甘油磷酸胆碱在体内和体外均可促进大鼠大脑皮层中的蛋白激酶C转位。

PKC translocation in rat brain cortex is promoted in vivo and in vitro by alpha-glycerylphosphorylcholine, a cognition-enhancing drug.

作者信息

Govoni S, Battaini F, Lucchi L, Pascale A, Trabucchi M

机构信息

Institute of Pharmacological Sciences, University of Milan, Italy.

出版信息

Ann N Y Acad Sci. 1993 Sep 24;695:307-10. doi: 10.1111/j.1749-6632.1993.tb23072.x.

DOI:10.1111/j.1749-6632.1993.tb23072.x

PMID:8239301

Abstract

Protein kinase C (PKC) activity was measured in soluble and particulate fractions of rat individual brain areas after treatment with alpha-glycerylphosphorylcholine (GPC), a cognition-enhancing drug which promotes acetylcholine synthesis and release. The drug induced both in vivo and in vitro PKC translocation. In vivo, an increase of particulate PKC activity was observed 1 hour following the acute oral administration of a behaviorally active dose (600 mg/kg); the effect was transient. In vitro, GPC promoted PKC translocation in cortical slices at concentrations as low as 50 nM; the concentration-response curve was bell shaped. The increased PKC activity may be related to the cortical effects of GPC.

摘要

在用α-甘油磷酸胆碱（GPC）处理后，对大鼠各个脑区的可溶性和颗粒性组分中的蛋白激酶C（PKC）活性进行了测定。GPC是一种促进乙酰胆碱合成和释放的认知增强药物。该药物在体内和体外均诱导PKC易位。在体内，急性口服行为活性剂量（600mg/kg）后1小时，观察到颗粒性PKC活性增加；该效应是短暂的。在体外，GPC在低至50nM的浓度下即可促进皮质切片中的PKC易位；浓度-反应曲线呈钟形。PKC活性增加可能与GPC的皮质效应有关。